@article{31547df16d634f599c8f982177a086fc,
title = "Discovery of VU2957 (Valiglurax): An mGlu 4 Positive Allosteric Modulator Evaluated as a Preclinical Candidate for the Treatment of Parkinson's Disease",
abstract = " Herein, we report the discovery of a novel potent, selective, CNS penetrant, and orally bioavailable mGlu 4 PAM, VU0652957 (VU2957, Valiglurax). VU2957 possessed attractive in vitro and in vivo pharmacological and DMPK properties across species. To advance toward the clinic, a spray-dried dispersion (SDD) formulation of VU2957 was developed to support IND-enabling toxicology studies. Based on its overall profile, VU2957 was evaluated as a preclinical development candidate for the treatment of Parkinson's disease. ",
keywords = "Parkinson's disease, Positive allosteric modulator (PAM), VU2957, metabotropic glutamate receptor 4 (mGlu )",
author = "Panarese, {Joseph D.} and Engers, {Darren W.} and Wu, {Yong Jin} and Bronson, {Joanne J.} and Macor, {John E.} and Aspen Chun and Rodriguez, {Alice L.} and Felts, {Andrew S.} and Engers, {Julie L.} and Loch, {Matthew T.} and Emmitte, {Kyle A.} and Castelhano, {Arlindo L.} and Kates, {Michael J.} and Nader, {Michael A.} and Jones, {Carrie K.} and Blobaum, {Anna L.} and Conn, {P. Jeffrey} and Niswender, {Colleen M.} and Hopkins, {Corey R.} and Lindsley, {Craig W.}",
note = "Funding Information: The authors would like to thank William K. Warren, Jr. and the William K. Warren Foundation who funded the William K. Warren, Jr. Chair in Medicine (to C.W.L.). Publisher Copyright: {\textcopyright} 2018 American Chemical Society. Copyright: Copyright 2019 Elsevier B.V., All rights reserved.",
year = "2019",
month = mar,
day = "14",
doi = "10.1021/acsmedchemlett.8b00426",
language = "English",
volume = "10",
pages = "255--260",
journal = "ACS Medicinal Chemistry Letters",
issn = "1948-5875",
publisher = "American Chemical Society",
number = "3",
}